Pyrrolidin-2-ones (I) of the formula: ##STR1## and their corresponding pyrrolidines (II) of the formula: ##STR2## wherein R.sup.1 =hydrogen, alkyl, substituted alkyl, aryl, substituted aryl, acyl or aroyl; R.sup.3 =hydrogen, alkyl, substituted alkyl, aryl or substituted aryl; R.sup.4 =aryl, substituted aryl, alkyl or substituted alkyl; R.sup.5 =hydrogen, alkyl, substituted alkyl, aryl or substituted aryl; and R.sup.5' =hydrogen, alkyl or substituted alkyl; include many known compounds exhibiting interesting CNS activity (Archivum Immunologiae et Therapiae Experimentalis 1975, 23, 733-751). Many of the compounds of Formula I above exhibit prostaglandin-like activity (Ger. Offen. No. 2,527,989).
The pyrrolidin-2-ones (I) have generally been prepared by ring closure of the corresponding 4-aminobutyric acid or ester (III) of the formula: ##STR3## and 4-halogeno-butyramide, by reaction of lactones with amines, or hydrolysis of 2-imino-pyrrolidines (Brit. Pat. No. 1,350,582 and U.S. Pat. No. 4,012,495).
These methods of producing compounds of Formula I and II were limited as to efficiency, type of substituents in the various positions and difficulty of producing pure stereo- and optically active isomers.